香加皮最大耐受量给药小鼠体内杠柳毒苷及苷元的代谢  

Study on Metabolism of Periplocin and Periplocin Aglycones of Cortex Periplocae Administered with the Maximum Tolerated Dose in Mice

作　　者：马志会[1] 张静[1] 周昆[1] 高秀梅[1] 

机构地区：[1]天津中医药大学中医药研究院,天津市中药药理重点实验室,天津300193

出　　处：《中药新药与临床药理》2010年第4期400-402,共3页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：“十一五”国家科技支撑计划重点项目(2006BAI14B01);天津市高等学校科技发展基金计划项目(20070302)

摘　　要：目的研究最大耐受量下香加皮中杠柳毒苷及苷元在小鼠体内的代谢规律。方法小鼠单次腹腔注射给予最大耐受量的香加皮水提物,高效液相色谱法测定给药后不同时间点血浆及心脏组织中杠柳毒苷及苷元的浓度。结果小鼠给药后,血浆中杠柳毒苷及杠柳毒苷苷元均出现多峰,其中杠柳毒苷在0～45 min时间段为吸收相,符合零级动力学,拟合方程为C=0.320 t,在45 min和120 min出现两个高峰,120～720 min时间段符合二室模型,t1/2α=1.694 min,t1/2β=344.049 min。在药后12 h内心脏组织中杠柳毒苷及杠柳毒苷苷元的含量相对稳定,没有显著降低。结论杠柳毒苷及苷元在体内存在肝肠循环,且苷元吸收较快;杠柳毒苷及苷元在心脏内有一定的蓄积。Objective To study metabolism of periplocin and periplocin aglycones of Cortex Periplocae administered with the maximum tolerated dose in mice. Methods Concentrations of periplocin and periplocin aglycones were determined by HPLC in plasma and heart at different time points after mice were given one-dose intraperitoneal injection of Cortex Periplocae water extract. Results After administration, the plasma concentration-time curve of periploein and periplocin aglycones in mice appeared several peaks. The absorbed phase of periplocin fitted to zero order kinetics within 0-45 min, and the equation was C=0.320 t. There were two peaks at the 45th rain and 120th rain. The curve fitted to a two-compartment model within 120-720 rain, t1/2α was 1.694 min, and t1/2β was 344.049 min. The concentration of periplocin and periplocin aglycones in heart was in a relatively stable level within 12 hours after administration. Conclusion There is an hepatoenteral circulation of periplocin and periplocin aglycones in mice, and periplocin aglycones can be absorbed faster. Periplocin and periplocin aglycones can be accumulated in heart.

关 键 词：香加皮 杠柳毒苷 杠柳毒苷苷元 代谢 

分 类 号：R285.5[医药卫生—中药学]